Conjugated Antisense Oligonucleotides

Manoharan, Muthiah; Tivel, Kathleen L.; Condon, Thomas P.; Andrade, Laura K.; Barber-Peoc'h, Isabelle; Inamati, Gopal B.; Shah, Shefali; Mohan, V.; Graham, Mark; Bennett, C. Frank; Crooke, Stanley T.; Cook, P. Dan

doi:10.1080/07328319708006147

Cited by 20 publications

(18 citation statements)

References 7 publications

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“…The uptake, and antisense activity of these ONAs are indeed greatly improved compared to underivatized analogs. 86,[95][96][97] Additionally and not surprisingly, such lipophilic conjugates proved to be more resistant toward nucleases, 94,95,98 and the resistance increases with the size of the aliphatic chain. 99 This strategy proved also successful with si-RNAs.…”

Section: Onas As Antisensementioning

confidence: 97%

Nucleoside, nucleotide and oligonucleotide based amphiphiles: a successful marriage of nucleic acids with lipids

et al. 2008

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Section: Onas As Antisensementioning

confidence: 97%

Nucleoside, nucleotide and oligonucleotide based amphiphiles: a successful marriage of nucleic acids with lipids

et al. 2008

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“…The former property is useful in the field of chip technology and diagnostics. [7][8][9][10] As an alternative, nucleosides in which the lipophilic group is attached to the nucleobase could also be incorporated into any position of an oligonucleotide. [2,3] The ability of oligonucleotides to permeate cell membranes by the introduction of lipidic structures into the oligonucleotides has been used in the development of antiviral compounds.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Nucleosides with 2′‐Fixed Lipid Anchors and Their Behavior in Phospholipid Membranes

Kaczmarek¹,

Brodersen²,

Bunge³

et al. 2008

Eur J Org Chem

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Various new nucleosides bearing one or two lipophilic groups at the 2′‐position have been synthesized. The lipophilic substituents were attached to a 2′‐hydroxy, 2′‐amino, or 2′‐thio function. These lipophilic nucleosides anchor in large unilamellar POPC vesicles serving as phospholipid membrane models. The insertion of these molecules into the membranes was investigated by NMR techniques. For comparison, nucleosides with two or three lipophilic groups at the 2′‐, 3′‐, or 5′‐positions have also been studied.(© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2008)

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“…In animal models, the P=S ODNs have a clear margin of safety, which has been borne out in clinical trials where systemic administration by intravenous infusion has been well tolerated. Formulation and/or chemical modification of antisense oligonucleotides can alter the pharmacokinetics and distribution (1,5,8,28 …”

Section: Future Directions Of Antisense Therapeuticsmentioning

confidence: 99%

Synthetic Oligonucleotides: The Development of Antisense Therapeutics

Monteith

Levin

1999

Toxicol Pathol

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Antisense therapeutics using synthetic oligodeoxynucleotides (ODNs) Antisense therapeutics are species specific because they are based on the genomic code. Although sequences may be relatively conserved among species, typical target regions for antisense therapeutics will differ by at least several bases between species. Therefore, to define pharmacologic effects, species-specific homologues of the human target must be identified and tested in the appropriate animal model. One exception is the use of human

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Conjugated Antisense Oligonucleotides

Cited by 20 publications

References 7 publications

Nucleoside, nucleotide and oligonucleotide based amphiphiles: a successful marriage of nucleic acids with lipids

Nucleoside, nucleotide and oligonucleotide based amphiphiles: a successful marriage of nucleic acids with lipids

Synthesis of Nucleosides with 2′‐Fixed Lipid Anchors and Their Behavior in Phospholipid Membranes

Synthetic Oligonucleotides: The Development of Antisense Therapeutics

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